References of 2-[4-[1-hydroxy-4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]butyl]
phenyl]-2-methylpropanoic acid
Title: Fexofenadine
CAS Registry Number: 83799-24-0
CAS Name: a,a-Dimethyl-4-[1-hydroxy-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]butyl]benzeneacetic acid
Synonyms: carboxyterfenadine; terfenadine carboxylate
Manufacturers' Codes: MDL-16455
Molecular Formula: C32H39NO4
Molecular Weight: 501.66
Percent Composition: C 76.61%, H 7.84%, N 2.79%, O 12.76%
Literature References: Nonsedating-type histamine H1-receptor antagonist. Prepn: A.A. Carr
et al., DE 3007498;
eidem, US 4254129 (1980, 1981 both to Richardson-Merrell). Identification as active metabolite of terfenadine,
q.v.: D. A. Garteiz
et al., Arzneim.-Forsch. 32, 1185 (1982). Synthesis: S. H. Kawai
et al., J. Org. Chem. 59, 2620 (1994). HPLC separation from terfenadine: K. Y. Chan
et al., J. Chromatogr. 571, 291 (1991); determn in biological fluids: A. Terhechte, G. Blaschke,
ibid. A 694, 219 (1995). Effects on cardiac K+ channels: D. Rampe
et al., Mol. Pharmacol. 44, 1240 (1993). Comparative analysis of cardiotoxic potential: J. A. Hey
et al., Arzneim.-Forsch. 46, 153 (1996). Clinical pharmacology in children: F. E. R. Simons
et al., J. Allergy Clin. Immunol. 98, 1062 (1996).
Properties: Crystals from methanol-butanone, mp 195-197° (Carr); also reported as white crystals from methanol, mp 142-143° (Kawai).
Melting point: mp 195-197° (Carr); mp 142-143° (Kawai)
Derivative Type: Hydrochloride
CAS Registry Number: 153439-40-8
Trademarks: Allegra (Aventis); Telfast (Aventis)
Molecular Formula: C32H39NO4.HCl
Molecular Weight: 538.12
Percent Composition: C 71.42%, H 7.49%, N 2.60%, O 11.89%, Cl 6.59%
Therap-Cat: Antihistaminic.
Keywords: Antihistaminic.